Liedholm H, Melander A
Clin Pharmacol Ther. 1986 Jul;40(1):29-36. doi: 10.1038/clpt.1986.135.
The influence of concomitant food intake on the bioavailability and presystemic primary conjugation of propranolol (80 mg) was studied in 11 healthy women. Food increased the maximum serum concentration and serum AUC of propranolol (P less than 0.05) and reduced those of conjugated propranolol (P less than 0.05). The mean AUC ratio of conjugated/unchanged propranolol was 13:1 in the fasting state but only about 6:1 in the nonfasting state (P less than 0.001). The time to maximum serum concentration and the t1/2 were not affected by food. There was no influence of food on any kinetic parameter of propranolol or conjugated propranolol when a slow-release formulation was used. We conclude that concomitant food intake can evoke a short-lasting, delivery rate-dependent inhibition of the presystemic primary conjugation of propranolol. This is one, but not the sole, mechanism by which food can enhance propranolol bioavailability.
在11名健康女性中研究了同时摄入食物对普萘洛尔（80毫克）生物利用度和系统前首步结合的影响。食物增加了普萘洛尔的最大血清浓度和血清药时曲线下面积（P<0.05），并降低了结合型普萘洛尔的上述指标（P<0.05）。结合型/未结合型普萘洛尔的平均药时曲线下面积比值在禁食状态下为13:1，但在非禁食状态下仅约为6:1（P<0.001）。达到最大血清浓度的时间和半衰期不受食物影响。当使用缓释制剂时，食物对普萘洛尔或结合型普萘洛尔的任何动力学参数均无影响。我们得出结论，同时摄入食物可引起对普萘洛尔系统前首步结合的短期、依赖释放速率的抑制。这是食物可提高普萘洛尔生物利用度的一种机制，但并非唯一机制。
